This invention is concerned with a new class of diazaditwistanes characterized by having a phenylalkyl group attached to either or both of the 2- and 9- positions of the complex ring system. The novel compounds have opiate receptor binding capability by virtue of which they are analgesic and antidiarrheal agents.
The diazaditwistane structure is relatively new appearing in the patent litereature first in U.S. Pat. No. 4,033,968 which disclosed a small class of analgesic compounds with an alkanoyl group at both the 2- and 9- positions. Molecular model studies comparing these compounds with enkephalins, and some of their analogs suggested that closer structural similarities with the enkephalins would be realized with the novel compounds of this invention.
Thus there is provided by the present invention a new class of diazaditwistanes characterized by a phenylalkyl group at either or both of the 2- and 9- positions which bind to opiate receptor sites and have central nervous system activities exemplified by analgesia.
There is also provided by this invention processes for preparing the novel compounds; pharmaceutical compositions employing the novel compounds as active ingredients; and a method of treating pain with the novel compounds and compositions of this invention.